Imatinib mesylate is chemically designated as 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl) pyrimidin-2-ylamino) phenyl]-benzamide methane sulfonate and its structural formula is
Imatinib is a protein-tyrosine kinase inhibitor, especially useful in the treatment of various types of cancer and can also be used for the treatment of atherosclerosis, thrombosis, restenosis, or fibrosis. Thus Imatinib is used for the treatment of non-malignant diseases. Imatinib is usually administered orally in the form of suitable salt, e.g., in the form of Imatinib mesylate.
Imatinib mesylate is a white to off white to brownish or yellow tinged crystalline powder. Imatinib mesylate is soluble in aqueous buffers ≦pH 5.5 but is very slightly soluble to in soluble in neutral/alkaline aqueous buffers. In non-aqueous solvents, the drug substance is freely soluble to very slightly soluble in dimethyl sulfoxide, methanol and ethanol, but is insoluble in n-octanol, acetone and acetonitrile.
Imatinib mesylate is sold under the brand name Gleevac® which is marketed by Novartis Pharmaceuticals. Gleevac® is available in tablets for oral administration in 100 and 400 mg strength. The inactive ingredients of Gleevac® are colloidal silicon dioxide (NF); crospovidone (NF); hydroxy propyl methyl cellulose (USP); magnesium stearate (NF); and microcrystalline cellulose (NF). Tablet coating: ferric oxide, red (NF); ferric oxide, yellow (NF); hydroxy propyl methyl cellulose (USP); polyethylene glycol (NF); and talc (USP).
U.S. Pat. No. 6,894,051 describes the process for the preparation of the α- and β-crystalline form of Imatinib mesylate, the α-crystalline form being hygroscopic.
US Patent Application no. 20100203133A1, relates to the formulation of Imatinib containing 30-80% w/w of Imatinib. The tablet described in US Patent Application no. 20100203133A1 is convenient to administer and provides a daily dose amount of Imatinib. However, there exists a need to develop a pharmaceutical composition which is more convenient and easier to swallow to provide a daily dose of Imatinib.